Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

A mixture of 5 (0.11g, 0.56mmol), DIPEA (0.10ml, 0.56mmol) and acetonitrile (3ml) was mixed with the 86 (0.10g, 0.56mmol) and then stirred at room temperature for overnight. The reaction was quenched by saturated NaHCO3 (aq.) and the mixture was extracted by ethyl acetate (30ml x 3). The residue was purified by flash column over silica gel (dichloromethane: methanol = 15: 1, Rf = 0.18) to afford 90 (0.06g, 30.80%) as a brown solid. 1H-NMR (300MHz, CDCl3): delta 1.15 (t, J= 7.2 Hz, 3H), 2.51 (q, J= 7.2 Hz, 2H), 2.64 (s, 4H), 3.01 (d, J= 7.2 Hz, 3H), 3.22 (t, J= 5.4 Hz, 4H), 5.30 (br, 1H), 5.74 (br, 1H), 6.88-6.94 (m, 2H), 7.11 (s, 1H), 7.35 (d, J= 9.0 Hz, 1H), 7.37-7.48 (s, 1H)., 115619-01-7

The synthetic route of 115619-01-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TAIPEI MEDICAL UNIVERSITY; YEN, Yun; LIOU, Jing-Ping; CHEN, Chun-Han; (70 pag.)WO2017/15400; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

/?-Toluenesulfonic acid monohydrate (0.304 g) was added to a mixture of 2-chloro-7-methyl-9-piperidin-4-yl-7,9-dihydro-8H-purin-8-one 4-methylbenzene- sulfonate (Method 38, 0.176 g), and 2-methoxy-4-(4-methylpiperazin-l-yl)aniline (Compound 46-3, page 138 in WO 04/080980, 0.089 g) in 4-methyl-2-pentanol (3 mL). The resulting suspension was heated at 16O0C for Ih in a microwave. The cooled solution was decanted and the residue was purified by RPetaPLC to provide the title compound as a brown gum (0.142 g, 57 %); 1H NMR: 1.94 (2H, m), 2.29 (6H, s), 2.60 (obscured, m), 3.12 (6H, m), 3.35 (obscured, m), 3.85 (3H, s), 4.52 (IH, m), 6.52 (IH, m), 6.66 (IH, d), 7.12 (2H, d), 7.40 (IH, s), 7.48 (2H, d), 8.06 (IH, d), 8.11 (IH, s); m/z: MH+ 453; EAA2: 5.36.

122833-04-9, 122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/24824; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The mixture of B (10.92g, 20.0mmol)), HATU (9.12g, 24.0mmol) and DIEA (3.87g, 30.0mmol) in DMF (lOOmL) was stirred at room temperature for 0.5h, then was added la (5.26g, 24.0mmol). The resulting mixture was stirred at room temperature for 0.5h and evaporated. The residue was purified by columnchromatography (EA:MeOH=5:l) to provide lb (12.43g, 83.2%)., 55121-99-8

55121-99-8 (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone 231408, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; XCOVERY HOLDING COMPANY, LLC; LIANG, Congxin; WO2012/48259; (2012); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 4 Preparation of 1-ethyl-4-(6-nitropyridin-3-yl)piperazine A mixture of 5-bromo-2-nitropyridine (1.02 g, 5.02 mmol) and 1-ethylpiperazine (1.71 g, 15.0 mmol) in N-methyl-2-pyrrolidinone (5 mL) was stirred at 120 C. for 3 h. After this time, the reaction was cooled to room temperature, poured into water (100 mL) and extracted with methylene chloride (2*100 mL). The combined organic layers were dried over sodium sulfate, filtered and the filtrate concentrated under reduced pressure. The resulting residue was purified by chromatography (silica, gradient, 1:49 methanol/methylene chloride to 1:9 methanol/methylene chloride) to afford 1-ethyl-4-(6-nitropyridin-3-yl)piperazine as a yellow solid: 1H NMR (400 MHz, DMSO-d6.) d 8.25 (d, J=2.8 Hz, 1H), 8.14 (d, J=9.2 Hz, 1H), 7.48 (dd, J=9.2, 2.8 Hz, 1H), 3.50-3.46 (m, 4H), 2.50-2.38 (m, 4H, merged with DMSO peak), 2.37 (q, J=7.2 Hz, 2H), 1.02 (t, J=7.2 Hz, 3H)., 5308-25-8

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Gilead Connecticut, Inc.; Blomgren, Peter A.; Currie, Kevin S.; Kropf, Jeffrey E.; Lee, Seung H.; Mitchell, Scott A.; Schmitt, Aaron C.; Xu, Jianjun; Zhao, Zhongdong; US2014/148430; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

4-[2-(4-tert-butoxycarbonylpiperazin-1-yl)thiazol-4-ylmethoxy]benzoic Acid A solution of tert-butyl 4-thiocarbamoylpiperazine-1-carboxylate (650 mg, 2.65 mmol) and 1,3-dichloroacetone (672 mg, 5.3 mmol) in 1,2-dichloroethane was treated with sodium bicarbonate (22 mg, 2.65 mmol). The reaction mixture was stirred at 70 C. for 18 hours and then diluted with chloroform. The dilution was washed with water and brine, dried over sodium sulfate and concentrated. Product was purified from the residue on a silica gel column, using ethyl acetate/hexanes (317) as eluent, to provide tert-butyl 4-(4-chloromethylthiazol-2-yl)piperazine-1-carboxylate (830 mg, 100% yield). H-NMR (dmso-d6): 6.92 (1H, s), 4.57 (2H, s), 3.40 (8H, m), 1.42 (9H, s)., 196811-66-2

196811-66-2 tert-Butyl 4-carbamothioylpiperazine-1-carboxylate 12093220, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AXYS PHARMACEUTICALS, INC.; US2002/86996; (2002); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To N, N-dimethylformamide (1000 ml) were added methyl 2-oxindole-6-carboxylate (100.0 g), benzoic acid methyl ester (78.3 g) and potassium carbonate (180.7 g) were added and stirred at room temperature for 3 hours. N- (4-aminophenyl) -N-methyl-2- (134.5g). After stirring at room temperature for 4 hours, the reaction mixture was poured into water (3000ml), stirred for 30 minutes, filtered and recrystallized from methylene chloride / methanol (10: 4 by volume) and dried to give 257.8g of crystals Compound. (89.7% yield).

262368-30-9, The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Beijing Kanglisheng Pharmaceutical Development Co., Ltd.; Cheng Gang; (12 pag.)CN104844499; (2017); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of carboxylic acid (50 mmol) in DMF (0.25 mL) in a 48 position Mettler Toledo XT reaction block was added PyBOP (50 mmol, 0.2 mL of 0.3 M solution in DMF) and TEA (75 mmol, 0.05 mL of 1.5 M solution in DMF) followed by the appropriate amine build blocks (55 mmol, 0.55 ml of 1 M solution in DMF). The reactions were stirred at rt 24 h and concentrated by GeneVac HT-4 to remove all reaction mixture including excess amine and DMF. The crude mixtures were dissolved in EtOAc (1 mL) and filtered through silica-packed short-column and washed with EtOAc (3 mL). The collected organic solution was concentrated in GeneVac HT-4 and dissolved in DMSO (1 mL). DMSO solution was subjected to HTAC for pre-purification analysis, purification, and final QC., 30459-17-7

As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference：
Article; Hwang, Jong Yeon; Attia, Ramy R.; Carrillo, Angela K.; Connelly, Michele C.; Guy, R. Kiplin; Bioorganic and Medicinal Chemistry Letters; vol. 23; 6; (2013); p. 1891 – 1895;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

1-(t-Butoxycarbonyl)-3-methylpiperazine To a cold (-5° C.) solution of 2-methylpiperazine (5.00 g, 0.05 mole) in 200 mL of CH2 Cl2 under Ar was added a solution of di-t-butyl dicarbonate (10.9 g, 0.05 mole) in 100 mL of CH2 Cl2 over 1 h. The resulting mixture was stirred at -5° C. for 1 h and then at r.t. for 2 h. The solution was then washed (H2 O), dried (Na2 SO4) and evaporated to give an oil which was chromatographed (SiO2 /ethyl acetate then ethyl acetate-MeOH-NH4 OH 10:1:0.1) to give the product (4.30 g, 43percent) as an oil. This material was used without further purification: 1 H nmr (200 MHz, CDCl3) delta 4.15-3.75 (br s, 2H), 3.0-2.6 (m, 4H), 2.47-2.35 (m, 1H), 1.48 (s, 9H), 1.08 (d, J=6.7 Hz, 3H).

109-07-9, The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Bristol-Myers Squibb Company; US5434154; (1995); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A NaOEt solution, prepared from sodium hydride (60% dispersion in mineral oil) (0.990 g, 26 mmol) and 100 mL EtOH, diethyl carbonate (9.00 mL, 74 mmol) and (S)-4-N-BOC-2-hydroxymethyl-piperazine (2.17 g, 10 mmol) was heated at 80 C. The reaction was cooled to RT and filtered. The filtrate was concentrated to dryness to give an off-white amorphous solid.

314741-40-7, 314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Amgen Inc.; US2006/199817; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

The compound (S) -5- (1 – ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (0.25g, 0.53mmol), 1-Boc-2- piperazine carboxylate(157mg, 0.64mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide Hydrochloride (153mg, 0.80mmol)and N- hydroxy-7-aza-benzotriazole (181mg, 1.33mmol) was dissolved in dichloromethane (20mL) Theconditions at 0 C to this solution was added dropwise N, N- diisopropylethylamine (0.37mL, 2.13mmol), 5Hstirred at room temperature, the solvent was removed, Concentrate was separated by column chromatography(eluent: Petroleumether / EtOAc (v / v) = 3/1), to give 260mg colorless viscous substance, yield: 70.

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics